Synthesis and c-Src inhibitory activity of imidazo[1,5- a]pyrazine derivatives as an agent for treatment of acute ischemic stroke

We studied novel c-Src inhibitors as potential therapeutic agents for acute ischemic stroke. Compound 14c· HCl demonstrated potent c-Src inhibitory activity, remarkable central nervous system (CNS) penetration, and significant neuroprotective efficacy in vivo in rat models. We synthesized and evalua...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2007-01, Vol.15 (2), p.868-885
Hauptverfasser:	Mukaiyama, Harunobu, Nishimura, Toshihiro, Kobayashi, Satoko, Ozawa, Tomonaga, Kamada, Noboru, Komatsu, Yoshimitsu, Kikuchi, Shinji, Oonota, Hideki, Kusama, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Acute Disease Animals Brain ischemia Brain Ischemia - complications c-Src Central nervous system (CNS) penetration CH–π interaction Crystallography, X-Ray Enzyme Inhibitors - blood Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Enzyme-Linked Immunosorbent Assay Humans Imidazo[1,5- a]pyrazine Imidazoles - chemical synthesis Imidazoles - pharmacology Indicators and Reagents Magnetic Resonance Spectroscopy Mass Spectrometry Models, Molecular Molecular Conformation Neuroprotective Agents - blood Neuroprotective Agents - chemical synthesis Neuroprotective Agents - pharmacology Pyrazines - chemical synthesis Pyrazines - pharmacology Rats Spectrophotometry, Infrared src-Family Kinases - antagonists & inhibitors Stroke - drug therapy Stroke - etiology Structure-Activity Relationship
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